200275
小檗碱 CRM 氯化物形式
A highly potent and selective oxysterol EBI2 (GPR183) agonist (Kd) = 450 pM in a saturation binding assay, and EC₅₀ = 140 pM over EC₅₀ = 2.1 nM for its enantiomer, 7β,25-OHC, in a GTP-γS binding assay).
别名:
黄连素
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所有图片(2)
About This Item
经验公式（希尔记法）:
C20H18ClNO4
CAS号:
分子量:
371.81
颜色索引号:
75160
Beilstein:
3836585
MDL编号:
UNSPSC代码:
12352200
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质量水平
方案
≥95% (NMR if no UV signal, HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
water: 1 mg/mL
DMSO: 10 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
COC1=C(C=[N+](CCC2=C3C=C4C(OCO4)=C2)C3=C5)C5=CC=C1OC.[Cl-]
InChI
1S/C20H18NO4.ClH/c1-22-17-4-3-12-7-16-14-9-19-18(24-11-25-19)8-13(14)5-6-21(16)10-15(12)20(17)23-2;/h3-4,7-10H,5-6,11H2,1-2H3;1H/q+1;/p-1
InChI key
VKJGBAJNNALVAV-UHFFFAOYSA-M
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一般描述
A highly potent and selective oxysterol EBI2 (GPR183) agonist (Kd) = 450 pM in a saturation binding assay, and EC50 = 140 pM over EC50 = 2.1 nM for its enantiomer, 7β,25-OHC, in a GTP-γS binding assay). Dose-dependently suppresses forskolin-induced cAMP accumulation in an EBI2-expressing SK-N-MC/CRE-β-galactosidase cell line (IC50 = 2 nM), but not in control cells. Stimulates migration of LPS-activated spleen B-cells and anti-CD3/CD28-activated CD4+ T-cells in a dose-dependent manner. In addition, pharmacological inhibition of its biosynthesis in vivo by Clotrimazole, a CYP7B1inhibitor, promotes the migration of adoptively transferred pre-activated B cells to the T/B boundary, mimicking the phenotype of pre-activated B cells in EBI2-deficient mice.
应用
肥大细胞中肝素的荧光染色
生化/生理作用
一种抗生素特性较弱的生物碱。MDR外排泵的底物。小檗碱的抗微生物活性可通过MDR抑制剂5'-甲氧基氢化物（5'-MHC）加强。小檗碱可上调肝癌细胞中Pgp的表达。用小檗碱进行治疗可能会减少化学治疗药物的积累。
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
其他说明
Kinm. B., et al. 2011, Brit. Journ. Pharm.164, 106.
Kong, W., et al. 2004, Nature Med.10, 1344.
Dimlich, R. et al. 1980, Stain Technol.55, 217.
Kong, W., et al. 2004, Nature Med.10, 1344.
Dimlich, R. et al. 1980, Stain Technol.55, 217.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Yingying Kou et al.
Frontiers in pharmacology, 11, 616251-616251 (2020-12-29)
Gastric cancer is one of the most common malignancies ranks as the second leading cause of cancer-related mortality in the world. Cisplatin (DDP) is commonly used for gastric cancer treatment, whereas recurrence and metastasis are common because of intrinsic and
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